Brief Story on Prostaglandins, Inhibitors of their Synthesis, Hematopoiesis, and Acute Radiation Syndrome

Höfer, Milan; Hoferová, Zuzana; Falk, Martin

doi:10.3390/molecules24224019

Cited by 9 publications

(2 citation statements)

References 68 publications

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“…The feature is involved in capsaicin, a TRPV1 channel agonist, and an 8% capsaicin patch (Qutenza) has been approved for the treatment of chronic pain in clinics [ 42 ]. Analgesic activities produced by a direct desensitization of nociceptive neurons might reduce side effects including gastrointestinal erosions, renal and hepatic insufficiency which are commonly associated with cyclooxygenase inhibitors [ 43 ]. As 10 μM (−)-NRG-DM did not affect TRPA1 currents, the neuronal desensitization could not be ascribed to its modulation on the channels ( Figure S1 ).…”

Section: Discussionmentioning

confidence: 99%

(−)-Naringenin 4′,7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels

Meng

Zhang

et al. 2022

Molecules

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(−)-Naringenin 4′,7-dimethyl ether ((−)-NRG-DM) was isolated for the first time by our lab from Nardostachys jatamansi DC, a traditional medicinal plant frequently used to attenuate pain in Asia. As a natural derivative of analgesic, the current study was designed to test the potential analgesic activity of (−)-NRG-DM and its implicated mechanism. The analgesic activity of (−)-NRG-DM was assessed in a formalin-induced mouse inflammatory pain model and mustard oil-induced mouse colorectal pain model, in which the mice were intraperitoneally administrated with vehicle or (−)-NRG-DM (30 or 50 mg/kg) (n = 10 for each group). Our data showed that (−)-NRG-DM can dose dependently (30~50 mg/kg) relieve the pain behaviors. Notably, (−)-NRG-DM did not affect motor coordination in mice evaluated by the rotarod test, in which the animals were intraperitoneally injected with vehicle or (−)-NRG-DM (100, 200, or 400 mg/kg) (n = 10 for each group). In acutely isolated mouse dorsal root ganglion neurons, (−)-NRG-DM (1~30 μM) potently dampened the stimulated firing, reduced the action potential threshold and amplitude. In addition, the neuronal delayed rectifier potassium currents (IK) and voltage-gated sodium currents (INa) were significantly suppressed. Consistently, (−)-NRG-DM dramatically inhibited heterologously expressed Kv2.1 and Nav1.8 channels which represent the major components of the endogenous IK and INa. A pharmacokinetic study revealed the plasma concentration of (−)-NRG-DM is around 7 µM, which was higher than the effective concentrations for the IK and INa. Taken together, our study showed that (−)-NRG-DM is a potential analgesic candidate with inhibition of multiple neuronal channels (mediating IK and INa).

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Section: Discussionmentioning

confidence: 99%

(−)-Naringenin 4′,7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels

Meng

Zhang

et al. 2022

Molecules

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“…The mode of action of flurbiprofen involves inhibiting cyclooxygenase enzymes (COX-1 and COX-2), which is reducing the synthesis of prostaglandins [ 3 ]. Prostaglandins play a key role in inflammation, pain, and fever.…”

Section: Introductionmentioning

confidence: 99%

Novel Flurbiprofen Derivatives as Antioxidant and Anti-Inflammatory Agents: Synthesis, In Silico, and In Vitro Biological Evaluation

Ivanov,

Manolov,

Bojilov

et al. 2024

Molecules

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In this study, we present the synthesis of five novel compounds by combining flurbiprofen with various substituted 2-phenethylamines. The synthesized derivatives underwent comprehensive characterization using techniques such as 1H- and 13C-NMR spectroscopy, UV-Vis spectroscopy, and high-resolution mass spectrometry (HRMS). Detailed HRMS analysis was performed for each of these newly created molecules. The biological activities of these compounds were assessed through in vitro experiments to evaluate their potential as anti-inflammatory and antioxidant agents. Furthermore, the lipophilicity of these derivatives was determined, both theoretically using the cLogP method and experimentally through partition coefficient (RM) measurements. To gain insights into their binding affinity, we conducted an in silico analysis of the compounds’ interactions with human serum albumin (HSA) using molecular docking studies. Our findings reveal that all of the newly synthesized compounds exhibit significant anti-inflammatory and antioxidant activities, with results statistically comparable to the reference compounds. Molecular docking studies further explain the observed in vitro results, shedding light on the molecular mechanisms behind their biological activities. Using in silico method, toxicity was calculated, resulting in LD50 values. Depending on the administration route, the novel flurbiprofen derivatives show lower toxicity compared to the standard flurbiprofen.

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Monounsaturated and polyunsaturated fatty acids: structure, food sources, biological functions, and their preventive role against noncommunicable diseases

Rincón‐Cervera

Bravo-Sagua

Freitas

et al. 2022

Bioactive Food Components Activity in Mechanistic Approach

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Brief Story on Prostaglandins, Inhibitors of their Synthesis, Hematopoiesis, and Acute Radiation Syndrome

Cited by 9 publications

References 68 publications

(−)-Naringenin 4′,7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels

(−)-Naringenin 4′,7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels

Novel Flurbiprofen Derivatives as Antioxidant and Anti-Inflammatory Agents: Synthesis, In Silico, and In Vitro Biological Evaluation

Monounsaturated and polyunsaturated fatty acids: structure, food sources, biological functions, and their preventive role against noncommunicable diseases

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